JP2006063074A5 - - Google Patents

Info

Publication number

JP2006063074A5

JP2006063074A5 JP2005219763A JP2005219763A JP2006063074A5 JP 2006063074 A5 JP2006063074 A5 JP 2006063074A5 JP 2005219763 A JP2005219763 A JP 2005219763A JP 2005219763 A JP2005219763 A JP 2005219763A JP 2006063074 A5 JP2006063074 A5 JP 2006063074A5

Authority

JP

Japan

Prior art keywords

pharmaceutical composition

group

composition according

hydroxymethyl

hydroxy

Prior art date

2005-07-29

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Pending

Links

• Espacenet
• Global Dossier
• Discuss

• NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 62
• 239000008194 pharmaceutical composition Substances 0.000 claims 46
• 108090001061 Insulin Proteins 0.000 claims 31
• 102000004877 Insulin Human genes 0.000 claims 31
• 101700032406 IAA Proteins 0.000 claims 24
• 239000003392 amylase inhibitor Substances 0.000 claims 24
• 101700007658 leg3 Proteins 0.000 claims 24
• 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 12
• 239000003623 enhancer Substances 0.000 claims 12
• 230000002708 enhancing Effects 0.000 claims 12
• 230000035945 sensitivity Effects 0.000 claims 12
• WLDBVPWSCOUGQI-ZMMVPWHFSA-N (2S,3R,4S,5S,6R)-2-[(2R,3S,4R,5R,6S)-4,5-dihydroxy-6-[(2R,3R,4R)-4-hydroxy-2-(hydroxymethyl)pyrrolidin-3-yl]oxy-2-(hydroxymethyl)oxan-3-yl]oxy-6-methyloxane-3,4,5-triol Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](C)O[C@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H](O[C@@H]2[C@H](NC[C@H]2O)CO)O[C@@H]1CO WLDBVPWSCOUGQI-ZMMVPWHFSA-N 0.000 claims 11
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 10
• 239000000203 mixture Substances 0.000 claims 10
• 230000000580 secretagogue Effects 0.000 claims 10
• XNCOSPRUTUOJCJ-UHFFFAOYSA-N diguanide Chemical compound NC(N)=NC(N)=N XNCOSPRUTUOJCJ-UHFFFAOYSA-N 0.000 claims 9
• 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 8
• 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 8
• 101700062901 DPP Proteins 0.000 claims 7
• 102100012353 DPP4 Human genes 0.000 claims 7
• 101700039720 DPP4 Proteins 0.000 claims 7
• 239000003112 inhibitor Substances 0.000 claims 7
• 230000002401 inhibitory effect Effects 0.000 claims 7
• 150000003839 salts Chemical class 0.000 claims 7
• 239000011780 sodium chloride Substances 0.000 claims 7
• 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 6
• 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 6
• 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 6
• 125000003277 amino group Chemical group 0.000 claims 6
• 239000003814 drug Substances 0.000 claims 6
• 150000002148 esters Chemical class 0.000 claims 6
• HYAFETHFCAUJAY-UHFFFAOYSA-N Pioglitazone Chemical compound N1=CC(CC)=CC=C1CCOC(C=C1)=CC=C1CC1C(=O)NC(=O)S1 HYAFETHFCAUJAY-UHFFFAOYSA-N 0.000 claims 4
• 229960005095 Pioglitazone Drugs 0.000 claims 4
• 125000004849 alkoxymethyl group Chemical group 0.000 claims 4
• 229940079593 drugs Drugs 0.000 claims 4
• WLDBVPWSCOUGQI-WPCAJUIMSA-N (2R,3R,4S,5S,6R)-2-[(2R,3S,4R,5R,6S)-4,5-dihydroxy-6-[(2R,3R,4R)-4-hydroxy-2-(hydroxymethyl)pyrrolidin-3-yl]oxy-2-(hydroxymethyl)oxan-3-yl]oxy-6-methyloxane-3,4,5-triol Chemical group O[C@@H]1[C@@H](O)[C@H](O)[C@@H](C)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H](O[C@@H]2[C@H](NC[C@H]2O)CO)O[C@@H]1CO WLDBVPWSCOUGQI-WPCAJUIMSA-N 0.000 claims 3
• 229960003105 Metformin Drugs 0.000 claims 3
• OELFLUMRDSZNSF-BRWVUGGUSA-N Nateglinide Chemical compound C1C[C@@H](C(C)C)CC[C@@H]1C(=O)N[C@@H](C(O)=O)CC1=CC=CC=C1 OELFLUMRDSZNSF-BRWVUGGUSA-N 0.000 claims 3
• 229960000698 Nateglinide Drugs 0.000 claims 3
• MFFMDFFZMYYVKS-SECBINFHSA-N Sitagliptin Chemical group C([C@H](CC(=O)N1CC=2N(C(=NN=2)C(F)(F)F)CC1)N)C1=CC(F)=C(F)C=C1F MFFMDFFZMYYVKS-SECBINFHSA-N 0.000 claims 3
• 125000000217 alkyl group Chemical group 0.000 claims 3
• 239000003795 chemical substances by application Substances 0.000 claims 3
• 125000001188 haloalkyl group Chemical group 0.000 claims 3
• 125000005843 halogen group Chemical group 0.000 claims 3
• XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical group CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims 3
• 230000001629 suppression Effects 0.000 claims 3
• 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 2
• 206010012601 Diabetes mellitus Diseases 0.000 claims 2
• YASAKCUCGLMORW-UHFFFAOYSA-N Rosiglitazone Chemical compound C=1C=CC=NC=1N(C)CCOC(C=C1)=CC=C1CC1SC(=O)NC1=O YASAKCUCGLMORW-UHFFFAOYSA-N 0.000 claims 2
• 150000001875 compounds Chemical class 0.000 claims 2
• 230000003449 preventive Effects 0.000 claims 2
• 229960004586 rosiglitazone Drugs 0.000 claims 2
• 230000004584 weight gain Effects 0.000 claims 2
• 235000019786 weight gain Nutrition 0.000 claims 2
• QGJUIPDUBHWZPV-VFGQHSGRSA-N (1R,3S,5R)-2-[(2S)-2-amino-2-[(5S,7R)-3-hydroxy-1-adamantyl]acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile Chemical compound C([C@@H](C1)C2)[C@@H](C3)CC1(O)CC23[C@H](N)C(=O)N1[C@H](C#N)C[C@H]2C[C@H]21 QGJUIPDUBHWZPV-VFGQHSGRSA-N 0.000 claims 1
• SYOKIDBDQMKNDQ-HHUWHTLVSA-N (2S)-1-[2-[[(5S,7R)-3-hydroxy-1-adamantyl]amino]acetyl]pyrrolidine-2-carbonitrile Chemical compound C([C@@H]1C[C@H](C2)CC(C1)(C1)O)C21NCC(=O)N1CCC[C@H]1C#N SYOKIDBDQMKNDQ-HHUWHTLVSA-N 0.000 claims 1
• HBBJLDPBYHSWOK-ZMMVPWHFSA-N (2S,3R,4S,5S,6R)-2-[(2R,3S,4R,5R,6S)-4,5-dihydroxy-6-[(2R,3R,4R)-4-hydroxy-2-(hydroxymethyl)pyrrolidin-3-yl]oxy-2-(hydroxymethyl)oxan-3-yl]oxy-6-(hydroxymethyl)oxane-3,4,5-triol Chemical compound OC[C@H]1NC[C@@H](O)[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)[C@@H](CO)O1 HBBJLDPBYHSWOK-ZMMVPWHFSA-N 0.000 claims 1
• 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
• -1 6-fluoro-6-deoxy-β-D-glucopyranosyl Chemical group 0.000 claims 1
• 210000004369 Blood Anatomy 0.000 claims 1
• XSEUMFJMFFMCIU-UHFFFAOYSA-N Buformin Chemical compound CCCC\N=C(/N)N=C(N)N XSEUMFJMFFMCIU-UHFFFAOYSA-N 0.000 claims 1
• 206010007572 Cardiac hypertrophy Diseases 0.000 claims 1
• WQZGKKKJIJFFOK-GASJEMHNSA-N D-Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
• 229960004580 GLIBENCLAMIDE Drugs 0.000 claims 1
• ZNNLBTZKUZBEKO-UHFFFAOYSA-N Glibenclamide Chemical group COC1=CC=C(Cl)C=C1C(=O)NCCC1=CC=C(S(=O)(=O)NC(=O)NC2CCCCC2)C=C1 ZNNLBTZKUZBEKO-UHFFFAOYSA-N 0.000 claims 1
• WIGIZIANZCJQQY-RUCARUNLSA-N Glimepiride Chemical compound O=C1C(CC)=C(C)CN1C(=O)NCCC1=CC=C(S(=O)(=O)NC(=O)N[C@@H]2CC[C@@H](C)CC2)C=C1 WIGIZIANZCJQQY-RUCARUNLSA-N 0.000 claims 1
• 206010020993 Hypoglycaemia Diseases 0.000 claims 1
• 108010016731 PPAR gamma Proteins 0.000 claims 1
• 102000012132 Peroxisome proliferator-activated receptor gamma Human genes 0.000 claims 1
• 229960003243 Phenformin Drugs 0.000 claims 1
• ICFJFFQQTFMIBG-UHFFFAOYSA-N Phenformin Chemical compound NC(=N)NC(=N)NCCC1=CC=CC=C1 ICFJFFQQTFMIBG-UHFFFAOYSA-N 0.000 claims 1
• XMSXOLDPMGMWTH-UHFFFAOYSA-N Rivoglitazone Chemical compound CN1C2=CC(OC)=CC=C2N=C1COC(C=C1)=CC=C1CC1SC(=O)NC1=O XMSXOLDPMGMWTH-UHFFFAOYSA-N 0.000 claims 1
• 229960004937 Saxagliptin Drugs 0.000 claims 1
• 108010026951 Short-Acting Insulin Proteins 0.000 claims 1
• 239000012190 activator Substances 0.000 claims 1
• 239000008280 blood Substances 0.000 claims 1
• 229960004111 buformin Drugs 0.000 claims 1
• 229960004346 glimepiride Drugs 0.000 claims 1
• 239000008103 glucose Substances 0.000 claims 1
• 201000001421 hyperglycemia Diseases 0.000 claims 1
• 230000002218 hypoglycaemic Effects 0.000 claims 1
• JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims 1
• 235000014655 lactic acid Nutrition 0.000 claims 1
• 239000004310 lactic acid Substances 0.000 claims 1
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
• 230000000291 postprandial Effects 0.000 claims 1
• 230000000069 prophylaxis Effects 0.000 claims 1
• 230000002829 reduced Effects 0.000 claims 1
• YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical compound OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 claims 1